Side Effects of obeticholic acid: A Synthesis of Findings from 27 Studies

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Original Abstract of the Article

Major research findings

Obeticholic acid (OCA) is a drug that activates the farnesoid X receptor (FXR), a bile acid receptor. OCA is being investigated as a potential treatment for liver diseases such as primary biliary cirrhosis (PBC) and nonalcoholic steatohepatitis (NASH). 19 , , 2 . OCA has shown promise in treating PBC, 6 , 4 , 26 , and has potential benefits for NASH. , 20 , 7 . However, OCA has been found to cause some side effects. 17 , , 2 , 8 , 7 , 23 , 15 , 9 , 18 .

Reasons for side effects

The side effects of OCA are thought to be caused by its effects on bile acid metabolism and lipid metabolism, which result from its activation of FXR. 17 , , 2 , 8 , 7 , 23 , 15 , 9 , 18 .

Common side effects

Itching

The most common side effect of OCA is itching. 17 , 2 , 8 , 9 , 18 . This is thought to be caused by OCA's activation of FXR, which can alter bile acid metabolism and activate a receptor called GPBAR1 that is involved in itching. 17 , 8 . Additionally, OCA may increase the risk of liver failure in PBC patients with cirrhosis. 2 .

Lowering of high-density lipoprotein (HDL) cholesterol

OCA can lower HDL cholesterol. 17 , , 2 , 7 , 18 . This is thought to be caused by OCA's activation of FXR, which can inhibit cholesterol synthesis in the liver. .

Increasing of low-density lipoprotein (LDL) cholesterol

OCA can raise LDL cholesterol. 17 , , 2 , 7 , 18 . This is thought to be caused by OCA's activation of FXR, which can inhibit cholesterol synthesis in the liver and reduce the clearance of LDL cholesterol. .

Liver side effects

OCA may have side effects on the liver. 5 , 18 . This is thought to be caused by OCA's activation of FXR, which can alter bile acid metabolism in the liver and put a strain on the liver. 5 . Additionally, OCA may increase the risk of liver failure in PBC patients with cirrhosis. 2 .

Gastrointestinal side effects

OCA may cause side effects in the gastrointestinal system. 9 . This is thought to be due to OCA's alteration of bile acid metabolism, which can affect the function of the gastrointestinal system. 9 .

Side effects management

Itching

Treatment for itching may include drug therapy, such as antihistamines or topical steroids. 14 . Lifestyle changes and adjustments to bathing methods can also be effective. 14 .

Lowering of high-density lipoprotein (HDL) cholesterol

Preventing a decrease in HDL cholesterol involves diet and exercise. . Drug therapy, such as cholesterol-lowering drugs, may also be used as needed. .

Increasing of low-density lipoprotein (LDL) cholesterol

Preventing an increase in LDL cholesterol involves diet and exercise. . Drug therapy, such as cholesterol-lowering drugs, may also be used as needed. .

Liver side effects

To prevent liver side effects, it is important to have regular liver function tests. 5 . It is also important to reduce the burden on the liver through lifestyle changes such as avoiding alcohol and limiting fatty foods. 5 .

Comparison between studies

Similarities in studies

Many studies have shown that OCA activates FXR, which affects bile acid metabolism and lipid metabolism in the liver. 17 , , 2 , 8 , 7 , 23 , 15 , 9 , 18 . These effects can lead to side effects such as itching, lower HDL cholesterol, and higher LDL cholesterol. 17 , , 2 , 7 , 18 .

Differences in studies

Studies have shown that the severity and frequency of OCA side effects vary. 17 , , 2 , 7 , 18 . This is thought to be due to differences in study design and participant characteristics. 17 , , 2 , 7 , 18 .

Cautions about real-life applications

OCA is a drug that can be effective for treating liver diseases such as PBC and NASH, but it also has the risk of side effects. 17 , , 2 , 8 , 7 , 23 , 15 , 9 , 18 . Therefore, it is important to follow your doctor's instructions carefully and be aware of any potential side effects if you are taking OCA. 17 , , 2 , 8 , 7 , 23 , 15 , 9 , 18 .

Current limitations of research

Research on the side effects of OCA is still not extensive. 17 , , 2 , 8 , 7 , 23 , 15 , 9 , 18 . Additionally, the side effects of OCA may vary depending on the individual patient. 17 , , 2 , 8 , 7 , 23 , 15 , 9 , 18 . Therefore, further research on the side effects of OCA is needed. 17 , , 2 , 8 , 7 , 23 , 15 , 9 , 18 .

Future research directions

New drugs and treatment methods are needed to reduce the side effects of OCA. 17 , , 2 , 8 , 7 , 23 , 15 , 9 , 18 . Research is also needed to understand the different mechanisms by which OCA causes side effects in different individuals. 17 , , 2 , 8 , 7 , 23 , 15 , 9 , 18 .

Conclusion

OCA is a drug that can be effective for treating liver diseases such as PBC and NASH, but it also has the risk of side effects such as itching, lower HDL cholesterol, and higher LDL cholesterol. 17 , , 2 , 8 , 7 , 23 , 15 , 9 , 18 . Therefore, it is important to follow your doctor's instructions carefully and be aware of any potential side effects if you are taking OCA. 17 , , 2 , 8 , 7 , 23 , 15 , 9 , 18 . Future research is expected to develop safer and more effective treatments. 17 , , 2 , 8 , 7 , 23 , 15 , 9 , 18 .

Keywords
Benefit Keywords
Regulated BA homeostasis
Tissue-specific targeting
1
Attenuated fibrosis
Improved liver function
Reduced alkaline phosphatase
2
Second-line therapy
Treatment of PBC
3
OCA efficacy
PBC treatment
4
Cholestasis treatment
5
PBC treatment
6
NASH treatment
7
Reduced fibrosis
Reduced steatosis
8
Liver fibrosis treatment
9
rPBC management
10
Inflammation relief
Lipid reduction
NASH treatment
11
NAFLD treatment
12
Treat NASH
13
ALF/ACLF prevention
Hepatitis E treatment
14
NASH treatment
Reduced pruritus
15
Improved liver health
16
Cholestatic liver disease treatment
Liver-related metabolic disorder treatment
17
Inflammation suppression
NASH treatment
18
Liver disease treatment
19
Gallstone dissolution
Improved liver health
20
Improved prostate health
21
Improved liver function
Liver recovery
Reduced fibrosis
22
Metabolic disease treatment
23
ASBT inhibitors
Cholestasis treatment
24
Immunomodulatory therapy
Improved autoimmune hepatitis treatment
25
Symptomatic management
Treatment options
26
Liver fibrosis treatment
27
Risk Keywords
Side effects
1
Liver failure
Pruritus
2
Drug-related deaths
Inappropriate use
3
Side effects
4
Liver toxicity
5
Liver decompensation
Pruritus
8
Abdominal pain
Constipation
Diarrhea
Fatigue
Headache
Nausea
Pruritus
9
Side effects
10
OCA side effects
11
Dyslipidemic effect
13
Cholestasis
Side effects
14
Potential side effects
15
HDL lowering
LDL increase
Liver toxicity
Pruritus
16
HDL reduction
LDL increase
Pruritus exacerbation
17
Cholelithiasis
Dyslipidemia
Liver toxicity
Moderate benefits
Pruritus
18
Cholesterol side effects
19
Prostatic side effects
21
FXR selectivity
23
ASBTi diarrhea
24
Glucocorticoid side effects
25
Side effects
26
Itching
Side effects
27
Literature analysis of 27 papers
Positive Content
26
Neutral Content
1
Negative Content
0
Article Type
1
1
1
9
27
1.

The regulation of tissue-specific farnesoid X receptor on genes and diseases involved in bile acid homeostasis.

Author: XiangDong, YangJinyu, LiuLu, YuHengyi, GongXuepeng, LiuDong

Regulated BA homeostasis
Tissue-specific targeting
Side effects

This review discusses the role of tissue-specific intestine/liver farnesoid X receptor (FXR) in regulating bile acid homeostasis. It highlights the potential of targeting tissue-specific FXR as a therapeutic strategy for treating enterohepatic and metabolic diseases.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

2.

Obeticholic Acid: An Update of Its Pharmacological Activities in Liver Disorders.

Author: FiorucciStefano, Di GiorgioCristina, DistruttiEleonora

Attenuated fibrosis
Improved liver function
Reduced alkaline phosphatase
Liver failure
Pruritus

Obeticholic acid (OCA) is a semisynthetic derivative of chenodeoxycholic acid (CDCA) that has been approved for the treatment of primary biliary cholangitis (PBC) and is being investigated for the treatment of nonalcoholic steatohepatitis (NASH). OCA activates FXR and GPBAR1/TGR5, but it can have side effects such as pruritus, HDL lowering, and LDL increasing.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

3.

Are Clinicians Ready for Safe Use of Stratified Therapy in Primary Biliary Cholangitis (PBC)? A Study of Educational Awareness.

Author: JopsonLaura, KhannaAmardeep, PetersonPatricia, RudellElaine, CorriganMargaret, JonesDavid

Second-line therapy
Treatment of PBC
Drug-related deaths
Inappropriate use

The use of obeticholic acid, a second-line therapy for primary biliary cholangitis (PBC), is discussed, highlighting the importance of appropriate and safe implementation of this new treatment option.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

4.

Real-world experience with obeticholic acid in patients with primary biliary cholangitis.

Author: D'AmatoDaphne, De VincentisAntonio, MalinvernoFederica, ViganòMauro, AlvaroDomenico, PompiliMaurizio, PicciottoAntonino, PalittiValeria Pace, RusselloMaurizio, StoratoSilvia, PigozziMarie Graciella, CalvarusoVincenza, De GasperiElisabetta, LleoAna, CastellanetaAntonino, PellicelliAdriano, CazzagonNora, FloreaniAnnarosa, MuratoriLuigi, FagiuoliStefano, NiroGrazia Anna, FelettiValentina, CozzolongoRaffaele, TerreniNatalia, MarzioniMarco, PellicanoRinaldo, PozzoniPietro, BaiocchiLeonardo, ChessaLuchino, RosinaFloriano, BertinoGaetano, VinciMaria, MorgandoAnna, VanniEster, ScifoGaetano, SaccoRodolfo, D'AntòMaria, BelliaValentina, BoldizzoniRoberto, CasellaSilvia, OmazziBarbara, PoggiGuido, CristoferiLaura, GerussiAlessio, RoncaVincenzo, VenereRosanna, PonzianiFrancesca, CannavòMaria, MussettoAlessandro, FontanaRosanna, LositoFrancesco, FrazzettoEvelise, DistefanoMarco, ColapietroFrancesca, LabancaSara, MarconiGiulia, GrassiGiuseppe, GalatiGiovanni, O'DonnellSarah Elizabeth, MancusoClara, MulinacciGiacomo, PalermoAndrea, ClaarErnesto, IzziAntonio, PicardiAntonio, InvernizziPietro, CarboneMarco, Vespasiani-GentilucciUmberto,

OCA efficacy
PBC treatment
Side effects

Obeticholic acid (OCA) was effective in treating primary biliary cholangitis (PBC) in patients who had an inadequate response to ursodeoxycholic acid. Response rates were 42.9% at 12 months, with patients with cirrhosis experiencing lower tolerability.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

5.

Opposite effects of the FXR agonist obeticholic acid on Mafg and Nrf2 mediate the development of acute liver injury in rodent models of cholestasis.

Author: CarinoAdriana, BiagioliMichele, MarchianòSilvia, FiorucciChiara, BordoniMartina, RoselliRosalinda, Di GiorgioCristina, BaldoniMonia, RicciPatrizia, MontiMaria Chiara, MorrettaElva, ZampellaAngela, DistruttiEleonora, FiorucciStefano

Cholestasis treatment
Liver toxicity

OCA, an FXR agonist, was found to exacerbate cholestasis and liver injury in rodent models. Inhibiting FXR and Mafg, or inducing Nrf2, effectively reversed the liver toxicity caused by OCA.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

6.

A Placebo-Controlled Trial of Obeticholic Acid in Primary Biliary Cholangitis.

Author: NevensFrederik, AndreonePietro, MazzellaGiuseppe, StrasserSimone I, BowlusChristopher, InvernizziPietro, DrenthJoost P H, PockrosPaul J, RegulaJaroslaw, BeuersUlrich, TraunerMichael, JonesDavid E, FloreaniAnnarosa, HohenesterSimon, LuketicVelimir, ShiffmanMitchell, van ErpecumKarel J, VargasVictor, VincentCatherine, HirschfieldGideon M, ShahHemant, HansenBettina, LindorKeith D, MarschallHanns-Ulrich, KowdleyKris V, Hooshmand-RadRoya, MarmonTonya, SheeronShawn, PencekRichard, MacConellLeigh, PruzanskiMark, ShapiroDavid,

PBC treatment

This study discusses the potential benefit of obeticholic acid, a farnesoid X receptor agonist, for patients with primary biliary cholangitis (PBC). The study emphasizes the importance of managing PBC due to the potential for progression to cirrhosis and death.

Clinical Trial, Phase IIIA Phase III trial is a trial that further rigorously verifies the efficacy and safety of a new drug or treatment, whose efficacy and safety have been confirmed in a Phase II trial, in a large number of patients, and evaluates whether it is superior to existing treatments.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Multicenter StudyResearch conducted in collaboration with multiple research institutions. It aims to collect a wide range of data and obtain more generalizable results.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

7.

Bile acid modulators for the treatment of nonalcoholic steatohepatitis (NASH).

Author: FiorucciStefano, BiagioliMichele, SepeValentina, ZampellaAngela, DistruttiEleonora

NASH treatment

GPBAR1 and FXR ligands have shown efficacy in preclinical models of nonalcoholic steatohepatitis (NASH) by reversing steatohepatitis and fibrosis.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

9.

Side effect profile of pharmacologic therapies for liver fibrosis in nonalcoholic fatty liver disease: a systematic review and network meta-analysis.

Author: LiYilin, LeiRong, LeiHonglin, XiongQin, XieFengjiao, YaoChengjiao, FengPeimin

Liver fibrosis treatment
Abdominal pain
Constipation
Diarrhea
Fatigue
Headache
Nausea
Pruritus

This network meta-analysis systematically compares the drug-related side effects of different pharmacological agents used for treating liver fibrosis in NAFLD. The analysis found that lanifibranor, liraglutide, semaglutide, cenicriviroc, MSDC-0602K, and obeticholic acid have the highest risk of side effects in patients with NAFLD.

Meta-AnalysisA statistical technique that integrates the results of multiple studies to draw more general conclusions about a particular issue.
Systematic ReviewA review that systematically collects, evaluates, and integrates relevant research to answer a specific research question.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

10.

Combination antiretroviral therapy improves recurrent primary biliary cholangitis following liver transplantation.

Author: LytvyakEllina, NiaziMina, PaiRohit, HeDaniel, ZhangGuangzhi, HübscherStefan G, MasonAndrew L

rPBC management
Side effects

Combination antiretroviral therapy, specifically tenofovir/emtricitabine-based regimens with lopinavir or raltegravir, was used to manage recurrent primary biliary cholangitis in two patients. It resulted in sustained biochemical and histological improvement but was associated with side effects.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

12.

Isotschimgine alleviates nonalcoholic steatohepatitis and fibrosis via FXR agonism in mice.

Author: LiJunxiao, LiuChuhe, ZhouZhenyu, DouBaokai, HuangJinwen, HuangLeilei, ZhengPeiyong, FanShengjie, HuangCheng

NAFLD treatment

Isotschimgine (ITG), a non-steroidal FXR selective agonist, was evaluated for its therapeutic effects on nonalcoholic steatohepatitis (NASH) and fibrosis in mice. ITG improved steatosis, inflammation, and fibrosis, suggesting its potential as a novel therapy for NASH and hepatic fibrosis.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

14.

Treatment of Hepatitis E.

Author: HuiWei, WeiLinlin

ALF/ACLF prevention
Hepatitis E treatment
Cholestasis
Side effects

This article provides an overview of the current treatment options for hepatitis E virus (HEV) infections.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

15.

Discovery of novel ketoxime ether derivatives with potent FXR agonistic activity, oral effectiveness and high liver/blood ratio.

Author: TangXuehang, NingMengmeng, YeYangliang, GuYipei, YanHongyi, LengYing, ShenJianhua

NASH treatment
Reduced pruritus
Potential side effects

This study reports the development of novel non-steroidal farnesoid X receptor (FXR) agonists that show potent FXR agonistic activities in vitro and effectively promote target gene expression in vivo. The compounds have a high liver/blood ratio, potentially reducing side effects associated with systemic FXR activation.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

16.

Nonsteroidal FXR Ligands: Current Status and Clinical Applications.

Author: GegeChristian, HambruchEva, HambruchNina, KinzelOlaf, KremoserClaus

Improved liver health
HDL lowering
LDL increase
Liver toxicity
Pruritus

This chapter discusses the historical and ongoing efforts in the identification and development of nonsteroidal FXR agonists for clinical use. FXR agonists have shown promising results in the treatment of liver disorders, but they can have side effects such as pruritus, HDL lowering, and LDL increasing.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

19.

Knocking on FXR's door: the "hammerhead"-structure series of FXR agonists - amphiphilic isoxazoles with potent in vitro and in vivo activities.

Author: GegeChristian, KinzelOlaf, SteeneckChristoph, SchulzAndreas, KremoserClaus

Liver disease treatment
Cholesterol side effects

The Farnesoid X Receptor (FXR) is a promising target for treating liver diseases. Obeticholic Acid (OCA), a bile acid analogue that activates FXR, has been used in clinical trials but can cause cholesterol-related side effects. This review explores the development of synthetic FXR agonists that are not bile acid-like.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

20.

The Pharmacology of Bile Acids and Their Receptors.

Author: FiorucciStefano, DistruttiEleonora

Gallstone dissolution
Improved liver health

This review discusses the history of bile acids and their receptors as therapeutic targets. It highlights the potential benefits and risks of FXR-targeted therapies, such as obeticholic acid (OCA), and discusses the ongoing research in this area.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

21.

Testosterone protects from metabolic syndrome-associated prostate inflammation: an experimental study in rabbit.

Author: VignozziLinda, MorelliAnnamaria, SarchielliErica, ComeglioPaolo, FilippiSandra, CellaiIlaria, ManeschiElena, SerniSergio, GacciMauro, CariniMarco, PiccinniMarie-Pierre, SaadFarid, AdoriniLuciano, VannelliGabriella B, MaggiMario

Improved prostate health
Prostatic side effects

Testosterone supplementation protected rabbit prostate from metabolic syndrome-induced alterations.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

24.

Systemic ASBT inactivation protects against liver damage in obstructive cholestasis in mice.

Author: KunstRoni F, de WaartDirk R, WoltersFrank, DuijstSuzanne, VogelsEsther W, BoltIsabelle, VerheijJoanne, BeuersUlrich, Oude ElferinkRonald P J, van de GraafStan F J

ASBT inhibitors
Cholestasis treatment
ASBTi diarrhea

Systemically acting ASBT inhibitors, which divert bile salts towards renal excretion, may offer advantages over non-absorbable ASBT inhibitors for treating cholestatic liver disorders. This could alleviate issues like diarrhea and reduced efficacy in patients with extensive cholestasis.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

26.

Disease-modifying therapies and symptomatic management for primary biliary cholangitis.

Author: PatelRoshni, PortoneGreta, LambertJoshua A, MakSau, AlrubaiyLaith

Symptomatic management
Treatment options
Side effects

Ursodeoxycholic acid and obeticholic acid are recommended for treating primary biliary cholangitis, while cholestyramine is used for pruritus. However, further research is needed for other therapies like fibrates and budesonide, and no licensed therapy exists for fatigue.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

27.

Disruption of TFGβ-SMAD3 pathway by the nuclear receptor SHP mediates the antifibrotic activities of BAR704, a novel highly selective FXR ligand.

Author: CarinoAdriana, BiagioliMichele, MarchianòSilvia, ScarpelliPaolo, ZampellaAngela, LimongelliVittorio, FiorucciStefano

Liver fibrosis treatment
Itching
Side effects

BAR704, a 3-deoxy-6-ethyl derivative of CDCA, is a highly selective steroidal FXR agonist that may be useful for treating liver fibrosis without causing side effects associated with obeticholic acid, the first in class of FXR ligands.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

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